ArticlePloS one2015
Bioactivity-guided fractionation of an antidiarrheal Chinese herb Rhodiola kirilowii (Regel) Maxim reveals (-)-epicatechin-3-gallate and (-)-epigallocatechin-3-gallate as inhibitors of cystic fibrosis transmembrane conductance regulator.
Article in PloS one, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed.
- Distinct CFTR Mutation Spectrum and Atypical Clinical Presentations in Chinese Patients with Cystic Fibrosis.International journal of molecular sciences · 2026Review
- Insights Into Effects of Natural Bioactive Components on Inflammatory Diseases in Respiratory Tract.Phytotherapy research : PTR · 2025Review
- Epigallocatechin-3-gallate inhibits the collagen accumulation of oral submucous fibrosis induced by arecoline.Frontiers in pharmacology · 2025Article
- Relationship among Chinese herb polysaccharide (CHP), gut microbiota, and chronic diarrhea and impact of CHP on chronic diarrhea.Food science & nutrition · 2023Review
- Bioactivity guided isolation and identification of phenolic compounds fromCurrent research in food science · 2022Article
- Simultaneous Determination of 78 Compounds ofBiochemistry research international · 2021Article
- Phytochemical, Antibacterial and Antioxidant Activity Evaluation ofMolecules (Basel, Switzerland) · 2020Article
- Rhodiosin and herbacetin inPharmaceutical biology · 2019Article
- Identification of antiplasmodial triterpenes from Keetia species using NMR-based metabolic profiling.Metabolomics : Official journal of the Metabolomic Society · 2019Article
- Therapeutic Effect and Mechanism Study ofEvidence-based complementary and alternative medicine : eCAM · 2019Article
- Bioactivity-Guided Fractionation of Pine Needle Reveals Catechin as an Anti-hypertension Agent via Inhibiting Angiotensin-Converting Enzyme.Scientific reports · 2017Article
- The decrease in number of splenic lymphocytes in mice fedCentral-European journal of immunology · 2017Article
- Discovery of Clinically Approved Agents That Promote Suppression of Cystic Fibrosis Transmembrane Conductance Regulator Nonsense Mutations.American journal of respiratory and critical care medicine · 2016Article
- Role of Quercetin in Modulating Chloride Transport in the Intestine.Frontiers in physiology · 2016Article
- Modulation of Chloride Channel Functions by the Plant Lignan Compounds Kobusin and Eudesmin.Frontiers in plant science · 2015Article
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7 authors.
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Abstract
Cystic fibrosis transmembrane conductance regulator (CFTR) is the principal apical route for transepithelial fluid transport induced by enterotoxin. Inhibition of CFTR has been confirmed as a pharmaceutical approach for the treatment of secretory diarrhea. Many traditional Chinese herbal medicines, like Rhodiola kirilowii (Regel) Maxim, have long been used for the treatment of secretory diarrhea. However, the active ingredients responsible for their therapeutic effectiveness remain unknown. The purpose of this study is to identify CFTR inhibitors from Rhodiola kirilowii (Regel) Maxim via bioactivity-directed isolation strategy. We first identified fractions of Rhodiola kirilowii (Regel) Maxim that inhibited CFTR Cl- channel activity. Further bioactivity-directed fractionation led to the identification of (-)-epigallocatechin-3-gallate (EGCG) as CFTR Cl- channel inhibitor. Analysis of 5 commercially available EGCG analogs including (+)-catechins (C), (-)-epicatechin (EC), (-)-epigallocatechin (EGC), (-)-epicatechin-3-gallate (ECG) and EGCG revealed that ECG also had CFTR inhibitory activity. EGCG dose-dependently and reversibly inhibited CFTR Cl- channel activity in transfected FRT cells with an IC50 value around 100 μM. In ex vivo studies, EGCG and ECG inhibited CFTR-mediated short-circuit currents in isolated rat colonic mucosa in a dose-dependent manner. In an intestinal closed-loop model in mice, intraluminal application of EGCG (10 μg) and ECG (10 μg) significantly reduced cholera toxin-induced intestinal fluid secretion. CFTR Cl- channel is a molecular target of natural compounds EGCG and ECG. CFTR inhibition may account, at least in part, for the antidiarrheal activity of Rhodiola kirilowii (Regel) Maxim. EGCG and ECG could be new lead compounds for development of CFTR-related diseases such as secretory diarrhea.
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